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Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41.


ABSTRACT: A new series of N-carboxyphenylpyrrole ligands were designed using GeometryFit based on an X-ray crystal structure of gp41. The synthesized ligands showed significant inhibitory activities against HIV gp41 6-helix bundle formation, HIV-1 mediated cell-cell fusion and HIV-1 replication.

SUBMITTER: Wang Y 

PROVIDER: S-EPMC2818531 | biostudies-literature | 2010 Jan

REPOSITORIES: biostudies-literature

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Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41.

Wang Yong Y   Lu Hong H   Zhu Qiang Q   Jiang Shibo S   Liao Yun Y  

Bioorganic & medicinal chemistry letters 20091105 1


A new series of N-carboxyphenylpyrrole ligands were designed using GeometryFit based on an X-ray crystal structure of gp41. The synthesized ligands showed significant inhibitory activities against HIV gp41 6-helix bundle formation, HIV-1 mediated cell-cell fusion and HIV-1 replication. ...[more]

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